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Start Over Author "Xie, Saisai" Journal chemmedchem
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3. Gramicidin-S-Inspired Cyclopeptidomimetics as Potent Membrane-Active Bactericidal Agents with Therapeutic Potential.

Author

Hu C, Wen Q, Huang S, Xie S, Fang Y, Jin Y, Campagne R, Alezra V, Miclet E, Zhu J, and Wan Y

Subjects
Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents chemistry, Dose-Response Relationship, Drug, Gramicidin chemical synthesis, Gramicidin chemistry, Membrane Potentials drug effects, Microbial Sensitivity Tests, Molecular Conformation, Peptidomimetics chemical synthesis, Peptidomimetics chemistry, Structure-Activity Relationship, Anti-Bacterial Agents pharmacology, Bacteria drug effects, Gramicidin pharmacology, Peptidomimetics pharmacology
Abstract

Antimicrobial peptides (AMPs) are promising antibacterial agents often hindered by their undesired hemolytic activity. Inspired by gramicidin S (GS), a well-known cyclodecapeptide, we synthesized a panel of antibacterial cyclopeptidomimetics using β,γ-diamino acids (β,γ-DiAAs). We observed that peptidomimetic CP-2 displays a bactericidal activity similar to that of GS while possessing lower side-effects. Moreover, extensive studies revealed that CP-2 likely kills bacteria through membrane disruption. Altogether, CP-2 is a promising membrane-active antibiotic with therapeutic potential., (© 2020 Wiley-VCH GmbH.)

Published
2021
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